KR890008121A - Rhodanine Derivatives and Pharmaceutical Compositions - Google Patents

Abstract

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Description

Rhodanine Derivatives and Pharmaceutical Compositions

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Claims (11)

Rhodanine derivative of the following general formula (I) and its pharmaceutically acceptable salt. Wherein R ¹ is C ₁ -C ₆ alkyl or group — (CH ₂ ) _n COOR ³ , where n is an integer from 1 to 4 and R ³ is hydrogen or C ₁ -C ₆ alkyl; R ² is a group —CH═CH—R ⁴ or —CH ₂ —CH ₂ —R ⁴ , wherein R ⁴ is substituted or unsubstituted phenyl or substituted or unsubstituted 5-membered heterocyclic group. to be. The compound of claim 1, wherein R ¹ is a group — (CH ₂ ) _n COOR ³ , n is 2 or 3, and R ³ is hydrogen or C ₁ -C ₄ alkyl. The compound of claim 1, wherein R ² is a group —CH═CH—R ⁴ and R ⁴ is phenyl or C ₁ -C ₆ alkyl, C ₁ -C ₆ alkoxy, hydroxyl, halogen, carboxyl and carboxyl-, A substituted phenyl having at least one substituent selected from alkoxycarbonyl- or tetrazolyl-substituted alkoxy. The compound of claim 1, wherein R ² is a group —CH═CH—R ⁴ and R ⁴ is thienyl, halogen-substituted thienyl, or pyrrolyl. The compound of claim 1, wherein R ² is a group —CH ₂ —CH ₂ —R ⁴ and R ⁴ is phenyl optionally substituted by C ₁ -C ₆ alkyl, C ₁ -C ₆ alkoxy or hydroxyl. A medicament having a chemical transporter inhibitory activity, characterized in that it contains, as an active ingredient, a rhodanine derivative of formula (I) or a pharmaceutically acceptable salt thereof, together with one or more pharmaceutically acceptable additives or excipients: Pharmaceutical composition. Wherein R ¹ is C ₁ -C ₆ alkyl or group — (CH ₂ ) _n COOR ³ , where n is an integer from 1 to 4 and R ³ is hydrogen or C ₁ -C ₆ alkyl; R ² is a group —CH═CH—R ⁴ or —CH ₂ —CH ₂ —R ⁴ , wherein R ⁴ is substituted or unsubstituted phenyl or substituted or unsubstituted 5-membered heterocyclic group. to be. The composition of claim 6, wherein R ¹ is a group — (CH ₂ ) _n COOR ³ , n is 2 or 3 and R ³ is hydrogen or C ₁ -C ₄ alkyl. The compound of claim 6, wherein R ² is a group —CH═CH—R ⁴ and R ⁴ is phenyl or C ₁ -C ₄ alkyl, C ₁ -C ₆ alkoxy, hydroxyl, halogen, carboxyl and carboxyl-, A composition of substituted phenyl having one or more substituents selected from alkoxycarbonyl- or tetrazolyl-substituted alkoxy. The composition of claim 6, wherein R ² is a group —CH═CH—R ⁴ and R ⁴ is thienyl, halogen-substituted thienyl or pyrrolyl. The composition of claim 6, wherein R ² is a group —CH ₂ —CH ₂ —R ⁴ and R ⁴ is phenyl optionally substituted by C ₁ -C ₆ alkyl, C ₁ -C ₆ alkoxy or hydroxyl. A process for preparing the compound of claim 1 and a pharmaceutically acceptable salt thereof, characterized by reacting rhodanine of formula (II) with a ketone of formula (III). Wherein R ¹ is C ₁ -C ₆ alkyl or group — (CH ₂ ) _n COOR ³ , where n is an integer from 1 to 4 and R ³ is hydrogen or C ₁ -C ₆ alkyl; R ² is a group —CH═CH—R ⁴ or —CH ₂ —CH ₂ —R ⁴ , wherein R ⁴ is substituted or unsubstituted phenyl or substituted or unsubstituted 5-membered heterocyclic group. to be. ※ Note: The disclosure is based on the initial application.